Synthesis and anticancer evaluation of amide derivatives of imidazo-pyridines

Rani, Chekuri Sharmila; Reddy, Alugubelli Gopi; Susithra, E.; Mak, Kit‐Kay; Pichika, Mallikarjuna Rao; Sreenivasulu, Reddymasu; Rao, Mandava V. Basaveswara

doi:10.1007/s00044-020-02638-w

Cited by 23 publications

(8 citation statements)

References 73 publications

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“…These molecules are stable at room temperature and cost effective ( 12 ). It has been previously evaluated that amide derivatives exhibit effective anticancer properties against various cancer cell lines, such as breast cancer (MCF-7 and MDA-MB-231), lung cancer (A549), and prostate cancer (DU-145) ( 28 ). Similarly, our synthesized analogs (α-AAA-A and α-AAA-B) showed cytotoxic effects against HL-60 and K562 cancer cells, which varied depending on concentrations of the molecules used.…”

Section: Discussionmentioning

confidence: 99%

Biologically Active α-Amino Amide Analogs and γδ T Cells—A Unique Anticancer Approach for Leukemia

et al. 2021

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Advanced stage cancers are aggressive and difficult to treat with mono-therapeutics, substantially decreasing patient survival rates. Hence, there is an urgent need to develop unique therapeutic approaches to treat cancer with superior potency and efficacy. This study investigates a new approach to develop a potent combinational therapy to treat advanced stage leukemia. Biologically active α-amino amide analogs (RS)-N-(2-(cyclohexylamino)-2-oxo-1-phenylethyl)-N-phenylpropiolamide (α-AAA-A) and (RS)-N-(2-(cyclohexylamino)-2-oxo-1-phenylethyl)-N-phenylbut2-enamide (α-AAA-B) were synthesized using linear Ugi multicomponent reaction. Cytotoxicities and IC50 values of α-AAA-A and α-AAA-B against leukemia cancer cell lines (HL-60 and K562) were analyzed though MTT assay. Cytotoxic assay analyzed percent killing of leukemia cell lines due to the effect of γδ T cells alone or in combination with α-AAA-A or α-AAA-B. Synthesized biologically active molecule α-AAA-A exhibited increased cytotoxicity of HL-60 (54%) and K562 (44%) compared with α-AAA-B (44% and 36% respectively). Similarly, α-AAA-A showed low IC50 values for HL-60 (1.61 ± 0.11 μM) and K562 (3.01 ± 0.14 μM) compared to α-AAA-B (3.12 ± 0.15 μM and 6.21 ± 0.17 μM respectively). Additive effect of amide analogs and γδ T cells showed significantly high leukemia cancer cell killing as compared to γδ T cells alone. A unique combinational therapy with γδ T cells and biologically active anti-cancer molecules (α-AAA-A/B), concomitantly may be a promising cancer therapy.

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Section: Discussionmentioning

confidence: 99%

Biologically Active α-Amino Amide Analogs and γδ T Cells—A Unique Anticancer Approach for Leukemia

et al. 2021

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“…27 Rani et al have synthesized a new set of amide derivative imidazopyridine ( 49a–49j ) compounds exhibiting anticancer activities when exposed to the breast (MCF-7 and MDA-MB-231) cancer, lung (A549) cancer, and prostate (DU-145) cancer cell lines via MTT assay (etoposide as the standard reference drug). Among those compounds, 49j showed the highest anticancer activities towards MDA-MB-231, MCF-7, A549 and DU-145 cell lines with the IC 50 values of 0.95 ± 0.039 μM, 0.021 ± 0.0012 μM, 0.091 ± 0.0053 μM, and 0.24 ± 0.032 μM, respectively 28 (Scheme 13).…”

Section: Pharmacologymentioning

confidence: 99%

Pyridine: the scaffolds with significant clinical diversity

et al. 2022

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“…), and antiparasitic (anti-leishmanial and anti-trypanosomal) properties [163][164][165][166][167][168][169][170][171][172][173][174]. Also, imidazopyridine derivatives are often studied as anticancer agents [175][176][177][178][179][180][181].…”

Section: Imidazopyridinesmentioning

confidence: 99%

Fused Pyridine Derivatives: Synthesis and Biological Activities

Istanbullu¹,

Bayraktar²,

Saylam³

2023

Exploring Chemistry With Pyridine Derivatives

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Five-membered heteroaromatic ring fused pyridine derivatives are of increasing interest in drug design and medicinal chemistry. The structural similarity of many drugs (especially antiviral and anticancer ones) with DNA bases such as adenine and guanine is a key factor to explain their effectiveness. Apart from these, it is also found in the structures of substances with antituberculosis, antibacterial, antifungal, anti-inflammatory, and antimalarial activities. Another advantage of this group of compounds is their positive contribution to solubility, polarity, lipophilicity, and hydrogen bonding capacity properties of the compounds they are incorporated into. In this chapter, various bioactivities of fused pyridine derivatives will be categorized and summarized.

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Synthesis and anticancer evaluation of amide derivatives of imidazo-pyridines

Cited by 23 publications

References 73 publications

Biologically Active α-Amino Amide Analogs and γδ T Cells—A Unique Anticancer Approach for Leukemia

Biologically Active α-Amino Amide Analogs and γδ T Cells—A Unique Anticancer Approach for Leukemia

Pyridine: the scaffolds with significant clinical diversity

Fused Pyridine Derivatives: Synthesis and Biological Activities

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